4-Methylesculetin

4-Methylesculetin is an orally active coumarin derivative, with potent anti-oxidant and anti-inflammatory activities. 4-Methylesculetin inhibits myeloperoxidase activity. 4-Methylesculetin protects bone resorption by reducing the elevated levels of bone-joint exoglycosidases, cathepsin-D and tartrate resistant acid phosphatases. 4-Methylesculetin ameliorats the upregulated non-enzymatic inflammatory markers like TNF-α, IL-1β, IL-6, COX-2 and PGE2, which is promising for research of inflammatory diseases^[1][2]. In Vivo:4-Methylesculetin (5 or 25 mg/kg, p.o., daily for 8 days) decreases MPO activity, reduces the colonic levels of IL-6 and counteracts GSH depletion, showing the intestinal antiinflammatory activity in Dextran sulfate sodium (DSS) rat model^[1].
4-Methylesculetin (25 and 50 mg/kg, p.o., once a day from 11th day to 25th day) significantly prevents the swelling, bone and cartilage destruction at the joint in arthritic rats^[2].